Trodelvy, also known as sacituzumab govitecan, has emerged as a promising treatment option for certain types of cancer, particularly metastatic triple-negative breast cancer (mTNBC), (HR)-positive and human epidermal growth factor receptor 2 (HER2)-negative breast cancer, and metastatic urothelial cancer. This medicine is supplied for injection: 180 mg lyophilized powder in single-dose vials for reconstitution. But what exactly is Trodelvy (sacituzumab govitecan), and how does it work?
Trodelvy is a novel antibody-drug conjugate (ADC) developed to target cancer cells specifically. Its mechanism of action involves a sophisticated combination of a monoclonal antibody and a cytotoxic drug payload. Let’s understand how Trodelvy exerts its anticancer effects.
Monoclonal Antibody Targeting:
Trodelvy consists of a monoclonal antibody called sacituzumab, which selectively binds to Trop-2 receptors that are overexpressed on the surface of cancer cells. Trop-2 is a transmembrane glycoprotein associated with cancer aggressiveness and poor prognosis. By targeting Trop-2, Trodelvy homes in on cancer cells while sparing healthy cells, minimizing off-target effects.
Internalization and Payload Delivery:
Once bound to Trop-2, Trodelvy is internalized into the cancer cell through receptor-mediated endocytosis. This internalization process facilitates the delivery of its cytotoxic payload, govitecan.
Cytotoxic Payload – Govitecan:
Govitecan is a topoisomerase I inhibitor, a class of drugs known for their ability to induce DNA damage and cell death. Specifically, govitecan inhibits topoisomerase I enzyme activity, leading to the accumulation of DNA breaks and ultimately triggering cancer cell apoptosis, or programmed cell death.
Enhanced Efficacy:
Trodelvy’s unique design offers several advantages over traditional chemotherapy. By delivering the cytotoxic payload directly to cancer cells via the monoclonal antibody, Trodelvy achieves targeted therapy, minimizing systemic toxicity and reducing side effects associated with conventional chemotherapy. Additionally, the internalization of Trodelvy into cancer cells enhances the concentration of govitecan within the tumor microenvironment, maximizing its anticancer efficacy.
Clinical Efficacy:
Clinical trials evaluating Trodelvy have demonstrated promising results in patients with metastatic triple-negative breast cancer and metastatic urothelial cancer who have previously received multiple lines of therapy. In these studies, Trodelvy has shown significant improvements in objective response rates, progression-free survival, and overall survival compared to standard treatment options.
Future Directions:
The success of Trodelvy in clinical trials has paved the way for its continued investigation in various cancer types and treatment settings. Ongoing research aims to explore its potential in combination therapies and earlier lines of treatment, as well as its efficacy in other Trop-2-expressing malignancies.
In conclusion, Trodelvy represents a breakthrough in cancer treatment with its innovative mechanism of action targeting Trop-2-expressing cancer cells. By harnessing the power of monoclonal antibodies and cytotoxic payloads, this treatment offers new hope for those battling aggressive and difficult-to-treat cancers. As research progresses, the full potential of Trodelvy in improving patient outcomes continues to unfold.
Reference:
https://www.trodelvy.com/
